藥理學
Endocrine drugs #Sermorelin: Growth hormone–releasing hormone #Somatostatin & dopamine agonist: for acromegaly #Bromocriptine: dopamine agonist, 不能通過中樞, 有周邊CV的功效 #Desmopressin: V2-selective vasopressin agonist #甘草酸中毒 (licorice poisoning): 抑制 11-beta-dehydrogenase & cortisol 的代謝, 作用在 mineralocorticoid receptor, 產生 mineralocorticoid 的功效. #Triamcinolone: synthetic corticosteroid. (口內膏常用) #Dexamethasone: synthetic corticosteroid. (抗發炎能力最強) #Fludrocortisone: synthetic mineralocorticoid. (鈉滯留能力最強) #Corticosteroid 不可用在 herpes simplex virus 造成的 dendritic dermatitis. #Dehydroepiandrosterone (DHEA): 可轉變為 androgen or estrogen. #Metyrapone: antiadrenal #Aminoglutethimide: 阻斷 cortisol and aldosterone 合成, 抑制 P450, aromatase (抑制 estrogen 合成) #Ketoconazole: 抑制 steroid 合成, also antifungus. #Spirolactone: diuretics, mineralocorticoid and androgen antagonis. #Mifepristone: RU486, progesterone and glococorticoid antagonist. Sex hormones #Diethylstilbestrol (DES): synthetic non-steroid estrogen. #Clomiphene: estrogen receptor antagonist, 抑制 estrogen 負回饋 #Tamoxifen: selective estrogen receptor modulator (SERM), for breast cancer #Raloxifene: SERM, partial agonist. for osteoporosis #Aminoglutethimide: aromatase inhibitor #Anastrozole: aromatase inhibitor, estrogen synthesis inhibitor #Desogestrel: a progestin. 抑制 estrogen 功效 #Mifepriston, mifepristol: RU486 #Danazol: 17alpha-alkylated androgen, antiestrogenic effect, for endometriosis, fibrocystic breast disease, hereditary angioedema #Buserelin: GnRH analog. #Ganirelix: GnRH antagonist #Cyproterone: androgen receptor antagonist #Flutamide, bicalutamide: androgen receptor antagonists, for metastatic prostate carcinoma #Finasteride: 5-alpha reductase inhibitor, for benign prostatic hyperplasia (BPH), 商品名: Propecia (柔沛), 治療雄性禿 #Minoxidil: 落健, 治療雄性禿 #Gossypol: male contraceptive, 破壞 seminiferous epithelium Thyroid #Levothyroxine: T4, 藥效恆定 #Liothyronine: T3, 藥效快, for myxedema coma (要先補充 cortisol) #Propylthiouracil (PTU), methimazole (MMI): antithyroid drugs, inhibit iodination and coupling. #Perchlorate (ClO4): ionic inhibitor, 降低甲狀腺中碘的濃度, for Grave's disease and amiodarone-induced thyrotoxicosis #Iodide + thiourylene + propanolol: for thyroid crisis #131-I: 初期因破壞甲狀腺引起 thyroid storm, 適用老年患者 #Lithium: 減少 thyroid 分泌 #Beta-blocker: 抑制 5'-deiodinase (for T4 -> T3), T3 減少 #急性高血鉀要立即補充鈣, 因為鈣可以緩解高血鉀的 cardiotoxic effects. #Gallium nitrate: 抑制骨的再吸收, 藥效快持久, for multiple myeloma #Dihydrotachysterol (DHT or DHT2): Vit. D, for hypoparathyroidism, osteoporosis, psoriasis #Calcitonin (CT): 抑制 osteoclast, 造成低血鈣, 低血磷, salmon CT 藥效較強, for Paget's disease #Etidronate, pamidronate: bisphosphonates, 抑制 osteoclast, for Paget's disease and osteoporosis #NaF: 促進 osteoblast, bone formation, for osteoporosis, 中毒會造成 osteosclerosis, dental fluorosis Osteoporosis # Primary: ## type I: 更年期後缺少 estrogen ## type II: long-term remodeling inefficiency # Secondary: 其他疾病, 用藥... DM # Type 1: (有 ketoacidosis) #* 補充 insulin #*# Lispro (超短效) #*# Regular (短效) #*# Lente, NPH (中效) #*# Ultralente, glargine (長效) # Type 2: ## Sulfonylurea: 阻斷 ATP-gated K+ channel, 刺激 B cell 分泌更多 insulin ##* Megltinides (repaglinide): 對 sulfonylurea 過敏者可用 ## Biguanides (metformin): 促進組織對 glucose uptake ## Thiazolinediones (glitazones): 減少 insulin resistance ## Alpha-glucosidase inhibitor (acarbose): 降低腸胃道對雙糖類的代謝與吸收 (減少 glucose 產生) Vitamins # Vit B1 (thiamine): (active form: thiamine pyrophostate (TPP)) #* 醣類代謝的 coenzyme #* Beriberi (腳氣病) #* Wernicke's encephalopathy, Korsakoff's syndrome: 飲酒過量 # Vit B2 (riboflavin): FMN, FAD 主要成分, 呼吸作用 coenzyme # Vit B3 (nicotinic acid, niacin): NAD, NADP 主要成分 #* Pellagra (癩皮病): 吃大量玉米造成 # Vit B5 (pantothenic acid): coenzyme A 的一部分 #* 懷孕前補充預防胎兒神經管缺陷 # Vit B6 (pyridoxine) #* drug interactions # Vit B12 (cobalamin, cyanocobalamin) #* B6, B12, folic acid 可降 homocystein #* 抗憂鬱藥物較有效 # Vit C (ascorbic acid): 抗氧化劑 #* Scurvy (壞血病) #* 膠原蛋白 (hydroxyproline) synthesis # Folic acid #* 預防胎兒神經管缺陷 # Vit A (retinol) #* Night blindness, keratomalacia (乾眼症) #* From beta-carotene # Vit K1 (phytonadione), K2 (menaquinone), K3 (menadione): #* 促進凝血因子製造: II, VII, IX, X #* In fava bean disease (蠶豆症, G6PD deficiency), K3 can induce hemolysis #* 早產兒 liver 發育不良, 易 Vit K deficiency # Vit E (alpha-tocopherol): 抗氧化劑 #* LDL 易被氧化 -> 心血管疾病 Minerals # Chromiun (鉻) #* Chromium piccolinate: 減肥藥 #* 缺少: glucose intolerance # Copper #* 慢性缺少: aneurysms of major arteries # Selenium (硒): 抗氧化劑 #* Keshan disease (克山症): 土壤缺乏硒 -> cardiomyopathy #* 中毒: 毛髮指甲脫落 # Zinc #* 缺乏: 發育遲緩, 不能性成熟 #* 與 Vit A 治療夜盲症 GI drugs Cimetidine, Ranitidine: H2 blocker Omeprazole: PPI, 不可逆結合 Dicyclomine, pirenzepine: M3 blocker Antacids: # Aluminum hydroxide: 可能造成 constipation # Calcium carbonate: 可能造成 milk-alkali syndrome # Magnesium 化合物: 可能造成 diarrhea Mucosal protective agents # Sucralfate # Bismuth # Carbenoxolone (甘珀酸) # Misoprostol: PGE1 analog, 亦可抑制胃酸分泌, 會造成 spontaneous abortion, 孕婦禁用 For Helicobacter pylori # Omeprazole + metronidazole (antimicrobial) + clarithromycin/amoxicillin # Bismuth + metronidazole + tetracycline/amoxicillin # Omeprazole + bismuth + metronidazole + tetracycline/amoxicillin Metoclopramide: dopamine + serotonin antagonist, prokinetics -> 促進胃排空 抗嘔吐 # Prochloperazine: dopamine antagonists # Ondansetron: 5HT3 (serotonin receptor) antogonist # Scopolamine: anticholinergic, for 暈車 # Diphenhydramine, meclizine: H1 antagonist # Tetrahydrocannabinol: 大麻主要成分, 止吐 瀉劑 # Bulk laxatives: methylcellulose, psyllium (車前), lactulose # Stool softener: mineral oil # Irratant: bisacodyl # Osmotic agent: magnesium salts. 止瀉劑 # Opiates: diphenoxylate # Absorbent powder: Kaolin # Coating agent: bismuth (for traveller's diarrhea) #* antimicrobial, antiproteolytic, increase prostaglandin synthesis # Somatostatin agonist: octreotide Gallstone drugs # Chenodiol = chenodeoxycholic acid: 人體自行合成的 bile acid ## 抑制 HMG-CoA -> 抑制 cholesterol 合成 ## 增加 bile acid 可溶解 chlesterol # Ursodiol = ursodeoxycholic acid: chenodiol 異構物 #* 不會負回饋抑制 bile acid 生成 # Methyl tert-butyl ether, monoctanoin: 有機溶劑, 灌入膽道 # GW4064: FXR activator, 促進 bile acid and phospholipid 合成 Pancreatic enzyme # 大量口服 Pancreatin + pancrelipase (from pig) + cimetidine (防止胃酸破壞酵素) #* Side effect: hyperuricemia Hepatitis B # recombinant vaccine # 母 HBeAg (+): hepatitis B immunoglobulin # Chronic: Lamivudine (neucleoside analogue) Hepatitis C Interferon alpha + ribavirin Esophageal variceal bleeding prevention: beta blocker (propanolol, nadolol) acute: # vasopressin (terlipressin) # somatostatin (octreotide) Surgery: banding, ligation, TIPS, liver transplantation Hepatic encephalopathy # Lactulose # Neomycin: 抑制腸內菌生長, 減少 NH3 生成 # 停用 diuretics Sympathomimetic Stimulants # Cocaine #* 抑制節前神經元 NE, DA, serotonin 的 reuptake #* Vasoconstriction -> 鼻中隔受損 # Amphetamine #* 加強 neurotransmitter 的釋放 #* Methamphetamine #* 降低食慾, 消除疲勞, 減少睡眠 #* Withdrawal: craving for drugs, lassitude, hyperphagia Supra-addictive effect: amphetamine, barbiturate 用相同酵素代謝, 同時服用使血中濃度上升 Psychedelics (hallucinogens, 迷幻藥) * MDMA (搖頭丸), LSD (搖腳丸) * 由 sympathomimetic stimulants 衍生 => 藥品種類超多 * 刺激 5-HT2 receptor * 幻覺 * 沒有戒斷症狀 Others # Ketamine: #* 麻醉用 #* 拮抗 Glutamate 的 NMDA receptor # Cannabis (大麻) #* Cannabinoids, THC (tetrahydrocannabinol) #* 輕微戒斷症狀 #* 止吐, also for glaucoma # Nicotine: #* 增強記憶, 減低侵略性, 減少體重增加 # Phencyclidine (PCP, 天使塵) #* 類似 ketamine 作用 戒毒 * 用作用機制相似, 長效, 口服 * 長效藥物停藥後, 較慢出現戒斷症狀, 程度也較輕 * Antagonist 讓戒斷症狀提早出現, 程度較嚴重 NSAIDs Mechanism: # 跟 COX 競爭 arachidonic acid 的 binding site, 可逆的 # Acetylation within the active site. esp. aspirin; 不可逆 COX-3: 在腦部特別多, 被 acetaminophen 抑制 功效: # Anti-inflammation # Analgesic # Anti-pyretic # Prophylaxis of heart disease, esp. aspirin # Prophylaxis of colorectal cancer # Treatment of Alzheimer's disease: 降低 amyloidogenic A beta-42 Adverse effects: # GI ulceration # Blockage of platelate aggregation => hemophilia contraindicated # Inhibition of renal function # Bronchospasm: because leukotriene 變多 => asthmatics contraindicated # Hypersensitivity: esp. aspirin => contraindicated # Inhibition of uterine motility Aspirin * Mechanism: acetylation of COX; irreversible * 低劑量只止痛, 高劑量才可抗發炎 * 抑制 TXA2 => 抑制凝血 * Adverse effect *# Gastric upset *# 中毒 => tinnitus (耳鳴) *# Hyperpnea -> respiratory alkalosis -> metabolic acidosis *# < 2g/day: 降低尿酸排除; > 4 g/day: 增加尿酸排除 * 感染病毒的幼兒禁用: 增加 Reye's syndrome; 改用 acetaminophen Selective COX-2 Inhibitor * Celecoxib, rofecoxib * 提高 heart attack 和 stroke 的危險 DMARDs TNF-alpha inhibitors: etanercept, infliximab Interleukin-1 antagonist: anakinra Nitric oxide-releasing NSAID: nitronaproxen: 可幫助胃功能恢復 Acetaminophen: at brain COX-3; 沒有抗發炎功用 *D-penicillamine For Gout Colchicine: # IV 注射造成 bone marrow suppression, renal failure, death # Diagnostic aid in gout # Mechanism: ## 減少 neutrophil 釋放 chemotactic factor, inflammatory cytokines ## Block tubulin polymeration -> 減少細胞 migration Uricosuric agents: 急性發作時無效 * Low dose: inhibit tubular secretion => 初始要併用 cochicin 以免痛風發作 * high dose: inhibit proximal tubular reabsorption # Probenecid #* 競爭腎小管的分泌, 維持 penicillin, cephalosporin, acyclovir, cyclosporine 血中濃度 # Sulfinpyrazone #* 預防慢性痛風 # Allopurinol #* 抑制 xanthine oxidase -> 抑制尿酸形成 #* 代謝物 oxypurinol 也有藥效 #* Esp. for chronic tophaceous gout Sedative-hypnotic Drugs Benzodiazepine (BDZ) * Reduction of anxiety; sedation: 低劑量 * Hypnosis; induction of sleep ** 減少進入睡眠的時間 ** 增加 stage 2 NREM sleep * 不能 antipsychotic, analgesic, 不影響 ANS * REM rebound: 忽然停藥 -> 焦慮不安, irritability, 想去睡覺 * Anesthesia: IV注射高劑量 * Anticonvulsant * Muscle relaxation: 多用 diazepam * Respiratory depression: 抑制延腦呼吸中樞 * 抑制 CV * 口服吸收速率決定於 lipophilicity (親脂性); CNS 作用速率決定於 lipid solubility (脂溶性) * 可通過 placental barrier, breast milk * 肝臟代謝, 腎臟排除 * Clorazepate: prodrug, 代謝物仍有活性, 較長效 副作用 # Daytime sedation, drowsiness # Psychologic and physiologic dependence Tolerance # metabolic: 對藥物代謝速率增加; BDZ 不會 # Pharmacodynamic: receptor down-regulation Flumazenil: BDZ competitive antagonist; for BDZ overdose; 不會拮抗 barbiturates Beta-carboline: inverse agonist; bind BDZ receptor but 不利於 Cl channel open Barbiturates Mechanism: # 影響 Na, K transport # 延長 GABA Cl channel opening duration # 高劑量 GABA-mimetic 作用: # CNS depression: no analgesic # Respiratory depression: 抑制對 CO2 & hypoxia 的反應 # 會 induce P-450 enzyme Phenobarbital: 長效 Newer Drugs Buspirone * selective anxiolytic effects * 不直接與GABA系統作用 * 對 5-HT 1A 作用 * 不會 rebound anxiety * 服藥一週以上才有效 Zolpidem: 助睡 Zaleplon: 減少進入睡眠時間 Nonbarbiturate sedatives # Chloral hydrate # Antihistamines # Ethanol Ethanol 代謝: (0級反應) # 低濃度 (< 100 mg/dL): alcohol dehydrogenase # 高濃度 (> 100 mg/dL): microsomal ethanol oxidizing system (MEOS) 作用: # CNS: relief of anxiety # Heart: acetaldehyde 的傷害; 抑制心肌 # Smooth muscle: vasodilation -> hypothermia; 子宮放鬆 長期影響: # GI tract: gastritis, bleeding # Liver: 女性較容易; 脂肪肝 -> 酒精性肝炎; NADH/NAD+ ratio 上升 -> 影響正常代謝; 用 pyruvate 還原 NADH 使 lactic acid 上升 # Pancreas: 急性胰臟炎 # CV: Dilated cardiomyopathy; 降低 CAD 機率 # Nervous: 對稱性周邊神經傷害; thiamin deficiency -> Wernicke-Korsakoff syndrome -> 外動眼肌麻痺 # Blood: 抑制 bone marrow; folic acid deficiency -> anemia; GI bleeding -> iron deficiency anemia # Endocrine: 減少 testosterone; 刺激 adrenocortical hormone 釋放 # Kidney: 抑制 antidiuretic hormone -> diuretic effect # Immune: 抑制 lung alveolar macrophage; 增強 liver, pancreas Kupper cells # Cancer: 製作, 發酵 -> carcinogen # Pregnancy: 流產死胎; fetal alcohol syndrome -> 發育中神經系統異常 Drug interaction * 不能與 acetaminophen 併用 * 使酵素活性降低, 肝臟血流供應減少 -> 某些藥物代謝慢: phenothiazine, vasodilator, aspirin 中毒 # 預防呼吸抑制 # 監測血糖 # 補充 thiamine # 補充電解質 戒酒 Alcohol withdrawal syndrome: 成年人 seizure 發作原因之一; 給予電解質, thiamine Disulfiram: 抑制 aldehyde dehydrogenase -> 難過 -> 停止喝酒 Naltrexone: opioid receptor antagonist Methanol 中毒 * > 50 mg/dL -> 血液透析, ethanol IV 注射 * 呼吸支持 * 活性碳無效 Fomepizole: 抑制 ADH Ethylene glycol 中毒 * 血液透析, ethanol IV 注射 * Formepizole Antipsychotics Chlorpromazine: phenothiazine, aliphatic 類; alpha 1 = 5-HT2 > D2 > D1, 副作用多, ocular complication Thioridazine: phenothiazine, piperidine 類;有 cardiac toxicity; 代謝產物藥效較高 Trifluoperazine, fluphenazine: phenothiazine, piperazine 類 Thiothixene: thioxanthene 類 Haloperidol: butyrophenone 類; D2 > D1 = D4 > alpha 1 > 5-HT2, but 嚴重的錐體外副作用 Clozapine: D4 = alpha 1 > 5-HT2 > D2 = D1; 過敏造成 agranulocytosis Sulpiride, pimozide: selective D2 antagonist Antimanic Drugs Li: # 只用在中低 mania # 調節 Na channel # 抑制 IP turnover -> 抑制 signal transduction * 無效時換用 valproate, carbamazipine Antidepressants * 連續吃好幾星期才有效果 * Postreceptor Hypothesis: 用藥後增加的神經傳導物質造成代償性突觸後神經元的活性down-regulation # Trycyclic #* 抑制 NE, 5-HT, DA reuptake ## Imipramine: also for 小孩尿床 # Selective Serotonin Reuptake Inhibitor (SSRI) #* 抑制 serotonin reuptake ## Fluoxetine: 百憂解 # Electroconvulsive therapy (ECT, 電極治療): 藥物都失效才考慮, like 重開機 Extrapyramidal syndrome # Acute dystonia # Akathisia (不能安坐) # Parkinsonism # Malignant syndrome # Tardive dyskinesia (遲緩性運動不能) Antiepileptic Drugs Sodium channel * S4 有很多帶正電的 Arginine * Na influx -> EPSP (扣板機) -> open -> inactivating particle 堵住孔道 -> repolarization Sodium channel blockers * Mechanism: 卡住孔道, 延長 inactivation * Use-dependent blockade: 癲癇發作越厲害, 越有效 # Phenytoin: 副作用大, 現不用 # Carbamazepine: 用最多; partial seizure 首選, also for trigeminal neuralgia # Lamotrigine Calcium channel blocker * 只有 Ethosuximide * For Absence seizure (小發作, 失神性發作) GABAergic enhancer * At GABA A receptor -> Cl influx -> hyperpolarization # Phenobarbital: barbiturates 類, 安全劑量窄, 易 overdose, 延長 channel open duration # Primidone: 在體內被代謝成 PEMA and phenobarbital # Diazepam: benzodiazepines 類, 較安全, 增加 channel open frequency, but 容易 tolerant ## Status epilepticus (癲癇重積狀態) 首選, 靜脈注射 ## Febrile convulsions 肛門塞劑, 嬰兒 # Gabapentin: maybe 促進 GABA 合成、釋放, not on GABA A; also for DM neuropathy # Tiagabine: 抑制 GABA 的 presynaptic reuptake # Vigabatrin: 抑制 GABA transaminase -> GABA 無法代謝 Multiple ionic current modifiers # Valproic acid: 抑制 Na & Ca channel, GABA enhancer, also for migraine # Topiramate: 抑制 Na channel; at GABA A receptor # Zonisamide: 抑制 Na & Ca channel Others # Acetazolamide: carbonic anhydrase 抑制劑, 利尿, but metabolic acidosis, 現少用 其他方面 # 意外懷孕 # Teratogenic # Vitamin K deficiency -> 要 folate supplement # Infantile spasms (點頭痙) 要用 glucocorticoids 而非 antiepileptic drugs # Febrile convulsions 首選 diazepam 肛門塞劑 Adverse effects || Carbamazepine || 視力模糊, 運動失調 || || Phenytoin || 眼球震顫, 牙齦增生, 毛髮增生, 缺乏 Vit K || || Ethosuximide || 嗜睡, 腸胃不適 || || Valproic acid || 食慾增加, 禿頭, 肝毒性, 畸胎 || || Acetazolamide || 代謝性酸中毒 || Antiparkinsonism Drugs Substantia nigra: (indirect 為主) # Direct pathway: 抑制 Globus pallidus (internal) # Indirect pathway: 促進 Globus pallidus (internal) -> 釋放 GABA -> 抑制 thalamus Dopamine receptors: # D1: ↑cAMP, ↑PIP2 # D2: ↓cAMP, ↓Ca, ↑K Levodopa: 進入中樞少, 其周邊副作用 # GI, CV, dyskinesias (運動困難), 不自主抽動, behavioral effects # 併用 carbidopa Levodopa: half life 短 -> 波動 -> akinesia <-> dyskinesia -> on-off phenomenon Carbidopa: 類似 L-dopa, 亦是 decarboxylase inhibitor, 不能通過BBB Sinemet: carbidopa/levodopa 1/10 or 1/4 Bromocriptine: # Ergot derivative dopamine receptor (D2) agonist # 副作用: pulmonary infiltrates, erythromelalgia (肢端紅痛病), 不能用在 psochosis pt. Amantidine: # Antiviral agent # 增加 dopamine 合成釋放, 抑制 reuptake # 副作用: livedo reticularis, postural hypotension Selegiline, rasagiline: Monoamine Oxidase B inhibitors, 不影響 catecholamines 代謝 Entacapone: COMT inhibitor, 只有 peripheral, short duration Tolcapone: COMT inhibitor, peripheral and central, long duration, 肝毒性 Antimuscarinic drugs: # 主要改善 tremor 和 rigidity, 對 bradykinesis 較無效 # 副作用: atropine-lkie, 睫狀肌麻痺 Skeletal Muscle Relaxants Neuromuscular Blocking Drugs * Nondepolarizing agents: 與 ACh 互相競爭 * Depolarizing agent: (只有 succinylcholine) *# Phase I (depolarizing): ACh agonist, posttetanic potentiation (強直後增強收縮) 會消失 *# Phase II (desensitizing): 堵住離子通道 * 副作用: respiratory paralysis, 與麻醉劑併用造成 malignant hyperthermia 造成肌肉放鬆的麻醉劑強度: isoflurane > sevoflurane > desflurane > enflurane tubocurarine: nondepolarizing, 亦促進 histamine -> hypotension 代謝快慢: ChE > 肝 > 腎 Spasmolytic Drugs # Diazepam: Benzodiazepine 類, GABA A receptor # Baclofen: GABA B agonist # Tizanidine: alpha-2 agonist # Gabapentin: antiepileptic, for multiple sclerosis # Dantrolene: 唯一直接作用在骨骼肌的解痙藥, 抑制 sacroplasmic reticulum 中 Ca 的釋放, for malignant hyperthermia # Botulinum toxin A: 抑制 ACh 的釋放 # Cyclobenzaprine: for acute muscle spasm, 在中樞 antimuscarinic Opioids 周邊作用機制: # 抑制 Adenylyl Cyclase # 促進 K channel -> hyperpolarization (at postsynaptic) # 抑制 Ca channel -> neurotransmitter 無法釋放 (at presynaptic) 中樞作用機制: # 抑制 GABA -> 抑制 pain inhibitory neuron Mechanisms of Tolerance: # Receptor desensitization # Receptor internalization # Up-regulation of cAMP system Not tolerated: # Miosis (縮瞳) -> pinpoint pupils # Constipation # Convulsion # Antagonist Adverse effects: # Increase intracranial pressure -> brain trauma 絕對禁用 # Histamine release # Tolerance or cross-tolerance # Abstinence syndrome (戒斷症狀) -> 毒癮發作要給 methadone (長效) Opioid toxication: -> 用 antagonist (naloxone, naltrexone) i.v. 治療 # Pinpoint pupils # Respiratory depression # Coma Agonists: # Morphine # Methadone # Fentanyl Partial agonists: # Butophanol Antagonists: # Naloxone # Naltrexone Anesthetics * halothane 反而會抑制 HR * desflurane 不能用在 asthma pt. * Thio-barbiturates (thiopental) 較短效 Non-barbiturate # Benzodiazepines (BDZ) #* Diazepam (Valium): 長效, 70hr #* Midazolam: 短效, 水溶性 Receptor affinity: lorazepam > midazolam > diazepam Flumazenil: BDZ competitive antagonist, 短效 Ketamine: rapid onset, on limbic system Propofol: * onset快, duration短, recovery好, but hypotension, 短暫呼吸抑制 * 溶劑cremophor 導致休克 * 促進 GABA 釋放 * 抑制 cholinergic receptor; physostigmine (anticholinesterase) can reverse it. 局部麻醉藥 Mech: 抑制 sodium channel Procaine: ester type, 易過敏, 第一個被合成 Lidocaine: amine type * 只有 cocaine 是 vasoconstriction * Bupivacaine 對 motor 的抑制較少, 較適合用在無痛分娩; but 心律不整機會高 * intercostal 注射較易中毒 Ropivacaine: duration 短, onset 長, 適合門診手術 Articaine: 牙醫常用 服藥時間間隔 * BID：早上九點，下午五點，共兩次 * q12h：早上九點，下午九點，共兩次 category:藥理學